Assay Detail
Binding
CHEMBL5381730
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of KIT (delta 560 to 576 residues) deletion/V654A double mutant autophosphorylation at Y703 in human GIST-430/654 harboring KIT (delta 560 to 576 residues) deletion mutation at exon 11 and imatinib resistance mutation V654A in exon 13
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | GIST-430/654 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Mast/stem cell growth factor receptor Kit (CHEMBL1936) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of M4205─A Highly Selective Inhibitor of KIT Mutations for Treatment of Unresectable Metastatic or Recurrent Gastrointestinal Stromal Tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.26 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.16 |
| CHEMBL4216467 | RIPRETINIB | 4.0 | 1 | 6.73 |
| CHEMBL1946170 | REGORAFENIB | 4.0 | 1 | 5.82 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 5.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4216467 | RIPRETINIB | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL1946170 | REGORAFENIB | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL941 | IMATINIB | IC50 | = | 4750.0 | nM | 5.32 |